Cardio tonic

1. Cardio Tonic
Prepared By:-
Mr. Arjun S. Dhawale
[Semester VII ]
Under the Guardian Teacher:-
Prof. Pravin Khatale.
[M.Pharm; Prof. S.G.S.P.S , IOP Akola]
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2. Content:-
1]Introduction.
2]Classification.
3]Structural activity relationship.
4]Mechanism of action.
5]Adverse effect.
6]Use.
7]Reference.
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3. Introduction :-
The cardiac glycosides are an important class of
naturally occurring drugs whose actions include both
beneficial and toxic effects on the heart. Their
desirable cardiotonic action is of particular benefit in
the treatment of congestive heart failure and
associated edema and their preparations have been
used as medicinal agents as well as poisons since
1500 B.C. This dual application serves to highlight
the toxic potential for this class of life-saving drugs.
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4. Source:-
1] D. purpurea eg. Digitoxine, ditoxine.
2] D. lanata eg. digitoxine, ditoxine, digoxine.
3] Strophanthus gratus (seed) eg. S.G.
4] Urginea (Scilla) eg. Proscillaridin A.
5] Bufo vulgaris (toad skin) eg. Bufotoxine.
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5. Most glycosides are obtained from leaves of the
foxglove, Digitalis purpurea or Digitalis lanata.
Classification of Cardiac Glycosides
1. Cardenolides .
2. Bufadenolides .
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6. Digoxin :-
Digitoxin :-
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7. SAR :-
C 17 lactone ring : imp for receptor bind.
Both saturated & unsaturated
C-D cis function is activity increase and A – B cis function
is decrease activity
C 17 double bond increase activity
-CH=CH-CH=NH at C 17 position higher activity .
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8. Steroidal Nucleus :-
C 14 OH group doesn't essential for activity .
Replacement of 3 OH /sugar by amino group 60 time more active .
Sugar portion:-
H- bonding is principle between sugar & enzyme.
It affects pharmacokinetic & pharmacodynamics parameter& not on
directly cardio tonic activity.
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9. Mechanism of Action :-
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10. MOA:-
1]Digitalis increase force of cardiac contraction by a direct action
independent innervations. It selectively bind to extra cellular face of
membrane associated NA+K+Atpase of myocardial fibers & inhibit
this enzyme.
2]Inhibition of this cation pump result in progressive accumulation of
NA +intracellularly
3]This indirectly result in intracellular Ca+ accumulation.
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11. Adverse Effects :-
1]Increase parasympathetic tone,
Hypokalemia.
2]Low safety margin.
3]Increase intracellular Ca++.
4]Decrease conduction .
5]Increase refractory period .
6]Increase ectopic automaticity.
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12. Uses :-
1] Conjestive cardiac failure .
2] Atrial arrhythmia .
Dose :-
Digoxin 0.25 mg tablet
0.05 mg/ml pediatric & 0.5 mg/2 ml inj.
Digi toxin 0.1 mg tab.
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13. Reference :-
1]Textbook of Organic Medicine Wilson and
Gisvold’s Pg.no. 656.
2] Medicinal Chemistry Cardiovascular Drugs by
Dr. Bahar Ahmed Pg.no.36.
3] Drug-Oriented Synthesis of Cardio tonic Steroids
by Will P. Kaplan.
4]Pharmacology Drugs acting on Cardiovascular
system by Dr. Gurudas Khilnani.
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14. Thank You
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